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Atom-by-atom tuning of the electrostatic potassium-channel modulator dehydroabietic acid

Silverå Ejneby, Malin, 1987- (author)
Linköpings universitet,Avdelning för neurobiologi,Medicinska fakulteten
Wu, Xiongyu, 1972- (author)
Linköpings universitet,Kemi,Tekniska fakulteten
Ottosson, Nina, 1984- (author)
Linköpings universitet,Avdelning för neurobiologi,Medicinska fakulteten
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Münger, E Peter, 1960- (author)
Linköpings universitet,Teoretisk Fysik,Tekniska fakulteten
Lundström, Ingemar, 1941- (author)
Linköpings universitet,Sensor- och aktuatorsystem,Tekniska fakulteten
Konradsson, Peter, 1957- (author)
Linköpings universitet,Kemi,Tekniska fakulteten
Elinder, Fredrik, 1966- (author)
Linköpings universitet,Avdelning för neurobiologi,Medicinska fakulteten
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 (creator_code:org_t)
2018-04-06
2018
English.
In: The Journal of General Physiology. - New York, United States : Rockefeller Institute for Medical Research. - 0022-1295 .- 1540-7748. ; 150:5, s. 731-750
  • Journal article (peer-reviewed)
Abstract Subject headings
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  • Dehydroabietic acid (DHAA) is a naturally occurring component of pine resin that was recently shown to open voltage-gated potassium (KV) channels. The hydrophobic part of DHAA anchors the compound near the channel’s positively charged voltage sensor in a pocket between the channel and the lipid membrane. The negatively charged carboxyl group exerts an electrostatic effect on the channel’s voltage sensor, leading to the channel opening. In this study, we show that the channel-opening effect increases as the length of the carboxyl-group stalk is extended until a critical length of three atoms is reached. Longer stalks render the compounds noneffective. This critical distance is consistent with a simple electrostatic model in which the charge location depends on the stalk length. By combining an effective anchor with the optimal stalk length, we create a compound that opens the human KV7.2/7.3 (M type) potassium channel at a concentration of 1 µM. These results suggest that a stalk between the anchor and the effector group is a powerful way of increasing the potency of a channel-opening drug.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Fysiologi (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Physiology (hsv//eng)

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